Herein, the phase-transfer reaction of quantum dots (QDs) with amine-terminated polyamidoamine (PAMAM) dendrimers with controllable ligand molar ratios was achieved. The unique properties of PAMAM allowed us to build up structurally and electrostatically stabilized water soluble QD complexes. Synthesized conjugates were characterized in terms of fluorescence and UV-Vis profiles, hydrodynamic size, number of surface dendrimer groups, and stability. Cytotoxic effects of conjugates for MCF-7, A-549 and HEP-G2 cancer cells were assessed based on cell viability using MTT assay. Cytotoxicity results were expressed as no observable adverse effect concentration (NOAEC), 50% inhibitory concentration (IC 50) and total lethal concentration (TLC) values (μM). Furthermore, HER2 receptor-mediated targeting efficiency of antibody labelled P/QDs conjugates was evaluated by successful staining of MCF-7 cells with bioconjugates. Uniquely, effective cell internalization was achieved with well-characterized antibody coupled P/QDs in contrast to antibody free P/QDs conjugates. Fluorescence microscopy images demonstrated that the designed PAMAM-derivatized QDs nanoparticles show great potential in the areas of cellular imaging and targeted therapy. © 2012 The Royal Society of Chemistry.